TC14012 TFA is a peptide-mimetic CXCR4 antagonist (IC50 = 19.3 nM) and CXCR7 agonist (EC50 = 350 nM) that promotes the recruitment of β-arrestin by CXCR7 and shares a ligand-binding surface for the CXCR4 and CXCR7 cores.

CXCR4-mediated HIV entry (U87.CD4.CXCR4 cells):19.3  nM, HIV infection (MT-4 cells):0.4  nM (EC₅₀)

In U87.CD4.CXCR4 cells infected with pseudotyped HIV-1 (X4-tropic strain), TC14012 TFA(1 μM) inhibited viral entry by over 95%. Further evaluation confirmed CXCR4-specific inhibition, with an IC₅₀ of 19.3 nM, indicating high specificity toward CXCR4-mediated HIV entry[1].TC14012 TFA was evaluated in an anti-HIV assay using MT-4 cells (HIV-infected, MTT assay, EC₅₀ = 0.4 nM). Cytotoxicity was assessed in uninfected MT-4 cells and human PBMCs (CC₅₀ >100 μM by MTT; >800 μM by trypan blue). TC14012 TFA demonstrated excellent anti-HIV activity and low cytotoxicity, with a selectivity index (SI) > 2,000,000[1].

In a CCl₄-induced liver fibrosis mouse model, UC-MSCs pretreated with TC14012 TFA were transplanted into mice. Treated cells showed enhanced anti-fibrotic effects compared to untreated UC-MSCs[2].